Histone Methyltransferase Inhibitor

Histone Methyltransferase Inhibitors (424):

Cat. No.	Product Name	Effect	Purity

HY-13803

Tazemetostat	Inhibitor	99.93%
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat also inhibits EZH1 with an IC₅₀ of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.

HY-13470

GSK126	Inhibitor	99.98%
GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM.

HY-15593

Pinometostat	Inhibitor	99.99%
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

HY-101563

GSK3326595	Inhibitor	99.83%
GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.

HY-13500

GSK343	Inhibitor	99.46%
GSK343, a chemical probe, is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.

HY-154812

Gintemetostat	Inhibitor	99.81%
Gintemetostat (KTX-1001) is a potent NSD2 inhibitor with an IC₅₀ ranging from 0.001 μM to 0.01 μM. As a piperidinyl-methyl-purineamine derivative, gintemetostat has potential applications in cancer research.

HY-W280124

PRMT9-IN-1	Inhibitor
PRMT9-IN-1 is a PRMT9 inhibitor. PRMT9-IN-1 can be used in the research of hematological cancer.

HY-176165

CDK9/EZH2-IN-1	Inhibitor
CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC₅₀: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC₅₀ values are 136.3, 171.3 and 315.7 nM, respectively).

HY-12186

3-Deazaneplanocin A hydrochloride	Inhibitor	99.98%
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities.

HY-10587

BIX-01294	Inhibitor	98.44%
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.

HY-139611

Navlimetostat	Inhibitor	99.40%
Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC₅₀ of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.

HY-136328

EZM0414 TFA	Inhibitor
EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC₅₀=18 nM in SETD2 biochemical assay; IC₅₀=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.

HY-13980

UNC0642	Inhibitor	99.86%
UNC0642, a chemical probe, is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

HY-N2019

Chaetocin	Inhibitor	99.58%
Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC₅₀ of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC₅₀ of 4 μM.

HY-101117

EED226	Inhibitor	99.56%
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC₅₀ of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.

HY-10442

3-Deazaneplanocin A	Inhibitor	99.97%
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.

HY-109108

Valemetostat	Inhibitor	99.84%
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

HY-128717A

GSK3368715 dihydrochloride	Inhibitor	99.96%
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC₅₀=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

HY-15227

EPZ004777	Inhibitor	99.00%
EPZ004777 is a potent, selective DOT1L inhibitor with an IC₅₀ of 0.4 nM.

HY-12727

EPZ015666	Inhibitor	99.83%
EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC₅₀ of 22 nM.

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